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Cefquinome liposome and preparation method thereof

A technology of cefquinol and cefquinol, which is applied in the field of cefquinol liposome and its preparation, can solve the problem of limited in vitro activity of Gram-negative anaerobic bacteria, inability to fully exert the drug effect and low bioavailability and other problems, to achieve broad industrialization prospects, improve bioavailability, and uniform particle size distribution.

Inactive Publication Date: 2014-02-19
HENAN SOAR VETERINARY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also active against penicillin-resistant staphylococci and enterococci, with limited in vitro activity against Gram-negative anaerobic bacteria
[0004] Cefquinol is easily soluble in organic solvents, but its water solubility is extremely poor, its bioavailability is low, and its efficacy cannot be fully exerted

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Cefquinol 25mg

[0037] Phosphatidylcholine 120mg

[0038] Octadecylamine 5mg

[0039] Cholesterol 50mg

[0040] Preparation method: dissolve the prescribed amount of phospholipids, cholesterol and octadecylamine in 4mL of ethanol (50% volume concentration), slowly inject into 8mL, 0.125mol / L ammonium sulfate solution at 50°C under magnetic stirring, and keep warm at 50°C Stir for 1 hour to completely volatilize the ethanol, place the probe in an ice bath and sonicate for 5 minutes to obtain blank liposomes. The obtained blank liposomes were placed in a dialysis bag, both ends were tied tightly, and dialyzed in 1000 mL, 0.9wt% NaCl solution for 24 hours to remove the ammonium sulfate in the liposome extracellular phase. Incubate the dialyzed blank liposome at 60°C, slowly add 1mL of an aqueous solution containing 25mg cefquinol under stirring, continue to incubate for 20min, and adjust the final volume to 10mL with 0.9wt% NaCl solution to obtain cefquinol liposome p...

Embodiment 2

[0042] Cefquinol 25mg

[0043]Phosphatidylcholine 120mg

[0044] Octadecylamine 5mg

[0045] Cholesterol 50mg

[0046] Chitosan 10mg

[0047] Preparation method: dissolve the prescribed amount of phospholipids, cholesterol and octadecylamine in 4mL of absolute ethanol, slowly inject into 8mL, 0.125mol / L ammonium sulfate solution under magnetic stirring at 50°C, keep stirring at 50°C for 1h to make no The water and ethanol were completely evaporated, and the probe was placed in an ice bath to sonicate for 5 minutes to obtain blank liposomes. The resulting blank liposomes were placed in a dialysis bag, the two ends were tied tightly, and dialyzed in 1000mL, 0.9wt% NaCl solution for 24h to remove the ammonium sulfate in the external aqueous phase of the liposomes. The dialyzed blank liposome was incubated at 60°C, slowly added 1 mL of an aqueous solution containing 25 mg cefquinol under stirring, and continued to be incubated for 20 min to obtain the cefquinol liposome. Diss...

Embodiment 3

[0049] Cefquinol 50mg

[0050] Phosphatidylcholine 300mg

[0051] PEG2000-DSPE 10mg

[0052] Cholesterol 100mg

[0053] Preparation method: Dissolve the prescribed amount of cefquinol, phospholipids, PEG2000-DSPE and cholesterol in 5mL ethanol (70% volume concentration), slowly inject into 10mL 0.9wt% NaCl solution at 50°C under magnetic stirring, 50 Insulate and stir at ℃ for 30 minutes to completely volatilize ethanol, place the probe in an ice bath and sonicate for 5 minutes to obtain cefquinol liposomes.

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PUM

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Abstract

The invention discloses cefquinome liposome. The cefquinome liposome comprises the following raw materials by weight: 0.01-50% of cefquinome or a salt thereof, 10-99.99% of phospholipid, 0-65% of cholesterol, 0-60% of deoxysodium cholate, 0-89.99% of anionic lipid, and 0-40% of an antioxidant. The invention further discloses a preparation method of the liposome. The cefquinome liposome researched by the invention has the advantages of excellent packaging rate, uniform particle size distribution, achievement of intravenous injection or local application standards, excellent stability and further improvement of stability through preparation of freeze-dried products. Moreover, the blank liposome-ammonium sulfate gradient medicine carrying preparation technique adopted by the invention is very suitable for large-scale industrial production, and has a wide industrialization prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cefquinol liposome and a preparation method thereof. Background technique [0002] Cefquinole, also known as cefquinome or cefquinome, and its trade name is Cobaxter, is the first animal-specific fourth-generation cephalosporin antibiotic developed by German Hoechst Animal Health Products Company. The molecular formula is: C 23 h 24 N 6 o 5 S 2 ·H 2 SO 4 , the molecular weight is 626. Cefquinol is off-white powder with stable properties. [0003] The mechanism of cefquinol's antibacterial action is to inhibit the synthesis of mucopeptides in the cell wall by competing with the mucopeptide synthase of bacteria, that is, the penicillin-binding protein, resulting in the defect of the bacterial cell wall, and a large amount of water rushes into the bacteria, causing the bacteria to swell, rupture, and die, and promote Sent from lysozyme activ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/546A61K47/36A61P31/04
Inventor 孙江宏付文力杨震豪
Owner HENAN SOAR VETERINARY PHARMA
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